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FX1

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Catalog No. T4089Cas No. 1426138-42-2

FX1 is an effective and selective BCL6 inhibitor (IC50: 35 μM).

FX1

FX1

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Purity: 97.59%
Catalog No. T4089Cas No. 1426138-42-2
FX1 is an effective and selective BCL6 inhibitor (IC50: 35 μM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$34In StockIn Stock
10 mg$52In StockIn Stock
25 mg$106In StockIn Stock
50 mg$166In StockIn Stock
100 mg$245In StockIn Stock
200 mg$356In StockIn Stock
1 mL x 10 mM (in DMSO)$38In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:97.59%
Appearance:Solid
Color:Red
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Product Introduction

Bioactivity
Description
FX1 is an effective and selective BCL6 inhibitor (IC50: 35 μM).
Targets&IC50
Bcl-6 BTB:35 μM
In vitro
FX1 markedly reduces recruitment of SMRT and BCOR to all 3 BCL6 target genes. There is little presence of SMRT at these loci in the BCL6-negative DLBCL cell line, which is not affected by FX1. After treatment with 50 μM FX1 for 6 hours, the superior potency of FX1 versus 79-6 in disrupting BCL6 binding to SMRT is evident when these small molecules are compared head to head in quantitative ChIP assays in DLBCL cells.
In vivo
Total B cell abundance is unaffected by FX1. FX1 significantly deplete GC B cells (GL7+FAS+B220+). Staining with B220 antibody reveals normal B cell follicular structures, whereas staining for the GC B cell-specific marker peanut agglutinin shows profound loss of GCs. The half-life is estimated to be approximately 12 hours. No signs of toxicity, inflammation, or infection are evident from H&E-stained sections of spleen, lung, gastrointestinal tract, kidney, heart, liver, and bone marrow of the fixed organs from mice treated with FX1 compare with the vehicle.
Cell Research
Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compared with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in a constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index [1].
Animal Research
Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. Cell viability of the drug-treated cells is normalized to their vehicle-treated controls, and the results are expressed as percentage viability. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compare with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index[1].
Chemical Properties
Molecular Weight368.82
FormulaC14H9ClN2O4S2
Cas No.1426138-42-2
SmilesOC(=O)CCN1C(=S)S\C(C1=O)=C1/C(=O)Nc2ccc(Cl)cc12
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25 mg/mL (67.78 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.71 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7113 mL13.5567 mL27.1135 mL135.5675 mL
5 mM0.5423 mL2.7113 mL5.4227 mL27.1135 mL
10 mM0.2711 mL1.3557 mL2.7113 mL13.5567 mL
20 mM0.1356 mL0.6778 mL1.3557 mL6.7784 mL
50 mM0.0542 mL0.2711 mL0.5423 mL2.7113 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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